The field of the invention is tobacco and antismoking products (deterrents) and the present invention is particularly concerned with agonists and antagonists to nicotine.
The state of the art of tobacco smoking deterrents may be ascertained by reference to U.S. Pat. Nos. 4,276,890 and 4,311,691 of FICHERA and U.S. Pat. No. 4,579,858 of FERNOE et al, the disclosures of which are incorporated herein by reference.
Fernoe et al are aware of the prior art nicotine containing chewing gums as disclosed in U.S. Pat. Nos. 865,026; 940,521; 3,877,468; 3,901,248 and 3,845,217 and state that it seems particularly difficult to find other smoking substitutes equivalent to or as effective as these nicotine containing chewing gums. U.S. Pat. No. 4,579,858 discloses a smoking substitute composition for application directly into the nose, consisting essentially of an aqueous solution of nicotine or a physiologically acceptable acid addition salt thereof, having a pH value of 2 to 6, containing 10 to 0.5% w/v of nicotine calculated as the free base, containing a nasally-acceptable thickening agent, having a viscosity not less than 100 centipose, and having about 0.5 to 5 mg nicotine per every 0.05 to 0.5 ml thereof and a method of diminishing the desire of a subject to smoke, which comprises the step of administering to the subject intranasally this smoking substitute composition.
The patents of Fichera disclose that the approach used by Fernoe et al has the difficulty that a physiological dependence upon nicotine remains and that unitl this dependence is overcome, the opportunity to resume smoking is very high. U.S. Pat. No. 4,311,691 defines a composition for inhibiting tobacco smoking comprising a gamma pyrone and an inert physiologically acceptable carrier capable of providing sustained release of the gamma pyrone in the mouth over a time period of at least ten (10) minutes, in unit dosage form containing from 20 mg to 300 mg of gamma pyrone per unit dose and a chewing gum composition for inhibiting tobacco smoking comprising a chewing gum base having particulate ethyl maltol distributed uniformly throughout, providing 100 mg to 300 mg ethyl maltol per stick of gum.
U.S. Pat. No. 4,276,890 defines the method of inhibiting tobacco smoking of smokers without physiological symptoms of nicotine withdrawal comprising smoking while awake during the waking hours of the day and administering to such a smoker 500 mg to 1500 mg total daily dose of ethyl maltol or maltol as a gamma pyrone divided into several incremental doses during the waking hours of the day, each incremental dose being retained in the smoker's mouth and released therein over a period of at least 10 minutes, for at least about 5 to 10 days, for a total of about 20 to 30 days or at least until there results either of a gradual decrease in the number of cigarettes smoked and the length of time they are smoked or until such point as the lowered tobacco consumption rate becomes obvious.
Fichera has contributed the discovery that the administration of maltol or ethyl maltol at appropriate dosage levels and rates, significantly reduces the tobacco consumption of habitual smokers.